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The (S)-enantiomer of 2-hydroxysaclofen is the active GABAB receptor antagonist in central and peripheral preparations

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dc.contributor.authorKerr, D.
dc.contributor.authorOng, J.
dc.contributor.authorDoolette, D.
dc.contributor.authorSchafer, K.
dc.contributor.authorPrager, R.
dc.date.issued1995
dc.description.abstractIn the guinea-pig isolated ileum, (RS)-(+/-)-baclofen induced a depression of cholinergic twitch contractions, reversibly and competitively antagonised by (S)-2-hydroxysaclofen (pA2 = 5.2 +/- 0.2), but not by (R)-2-hyroxysaclofen. The depression of excitatory field potentials by baclofen ( 5 mu M) in rat CA1 hippocampal slices was antagonised by (S)-2-hydroxysaclofen (100 mu m) (pA2 = 4.3), whilst in rat neocortex, (S)-2-hyroxysaclofen (50-500 mu M) antagonised the baclofen (10 mu M)-induced suppression of spontaneous discharges, the (R)-enantiomer being inactive. These results show that (S)-2-hydroxysaclofen is the active antagonist at central and peripheral GABAB receptors.
dc.identifier.citationEuropean Journal of Pharmacology, 1995; 287(2):185-189
dc.identifier.doi10.1016/0014-2999(95)00641-9
dc.identifier.issn0014-2999
dc.identifier.issn1879-0712
dc.identifier.orcidOng, J. [0000-0002-0958-460X]
dc.identifier.urihttp://hdl.handle.net/2440/5985
dc.language.isoen
dc.publisherElsevier
dc.rights© 1995 Elsevier Science B.V. All rights reserved
dc.source.urihttps://doi.org/10.1016/0014-2999(95)00641-9
dc.subjectGABAB receptor
dc.subject(RS)-(±)-Baclofen
dc.subject(S)-2-Hydroxysaclofen
dc.subject(R)-2-Hydroxysaclofen
dc.subjectIleum, guinea pig
dc.subjectHippocampus, rat
dc.subjectNeocortex, rat
dc.titleThe (S)-enantiomer of 2-hydroxysaclofen is the active GABAB receptor antagonist in central and peripheral preparations
dc.typeJournal article
pubs.publication-statusPublished

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